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PT536515E - NEW 7-SUBSTITUTED-9- (SUBSTITUTED AMINO) -6-DESMETIL-6-DEOXYETRACYCLINES - Google Patents

NEW 7-SUBSTITUTED-9- (SUBSTITUTED AMINO) -6-DESMETIL-6-DEOXYETRACYCLINES

Info

Publication number
PT536515E
PT536515E PT92114281T PT92114281T PT536515E PT 536515 E PT536515 E PT 536515E PT 92114281 T PT92114281 T PT 92114281T PT 92114281 T PT92114281 T PT 92114281T PT 536515 E PT536515 E PT 536515E
Authority
PT
Portugal
Prior art keywords
substituted
desmetil
deoxyetracyclines
new
substituted amino
Prior art date
Application number
PT92114281T
Other languages
Portuguese (pt)
Inventor
Joseph J Hlavka
Ving J Lee
Yakov Gluzman
Phaik-Eng Sum
Adma A Ross
Original Assignee
American Cyanamid Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=25092264&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PT536515(E) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by American Cyanamid Co filed Critical American Cyanamid Co
Publication of PT536515E publication Critical patent/PT536515E/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • C07C237/26—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/34—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42—Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
    • C07C2603/44—Naphthacenes; Hydrogenated naphthacenes
    • C07C2603/46—1,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Furan Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Hydrogenated Pyridines (AREA)
  • Saccharide Compounds (AREA)
  • Moulding By Coating Moulds (AREA)

Abstract

Novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.
PT92114281T 1991-10-04 1992-08-21 NEW 7-SUBSTITUTED-9- (SUBSTITUTED AMINO) -6-DESMETIL-6-DEOXYETRACYCLINES PT536515E (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US77157691A 1991-10-04 1991-10-04

Publications (1)

Publication Number Publication Date
PT536515E true PT536515E (en) 2002-05-31

Family

ID=25092264

Family Applications (1)

Application Number Title Priority Date Filing Date
PT92114281T PT536515E (en) 1991-10-04 1992-08-21 NEW 7-SUBSTITUTED-9- (SUBSTITUTED AMINO) -6-DESMETIL-6-DEOXYETRACYCLINES

Country Status (27)

Country Link
EP (1) EP0536515B1 (en)
JP (1) JP3186863B2 (en)
KR (1) KR100269072B1 (en)
CN (1) CN1048240C (en)
AT (1) ATE211128T1 (en)
AU (1) AU654049B2 (en)
BR (1) BR1100853A (en)
CA (1) CA2079692C (en)
CL (1) CL2004001623A1 (en)
CZ (2) CZ284209B6 (en)
DE (4) DE122006000058I1 (en)
DK (1) DK0536515T3 (en)
ES (1) ES2168254T3 (en)
FI (1) FI114911B (en)
HU (2) HU219973B (en)
IL (3) IL119590A (en)
LU (1) LU91279I2 (en)
MX (1) MX9205532A (en)
NL (1) NL300244I1 (en)
NO (3) NO301472B1 (en)
NZ (1) NZ244585A (en)
PL (4) PL175957B1 (en)
PT (1) PT536515E (en)
SG (1) SG52361A1 (en)
SK (2) SK284826B6 (en)
TW (1) TW275616B (en)
ZA (1) ZA927607B (en)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5284963A (en) * 1992-08-13 1994-02-08 American Cyanamid Company Method of producing 7-(substituted)-9-[(substituted glycyl)-amidol]-6-demethyl-6-deoxytetra-cyclines
US5328902A (en) * 1992-08-13 1994-07-12 American Cyanamid Co. 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
US5420272A (en) * 1992-08-13 1995-05-30 American Cyanamid Company 7-(substituted)-8-(substituted)-9-](substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
WO1995022529A1 (en) * 1994-02-17 1995-08-24 Pfizer Inc. 9-(substituted amino)-alpha-6-deoxy-5-oxy tetracycline derivatives, their preparation and their use as antibiotics
US8106225B2 (en) 1999-09-14 2012-01-31 Trustees Of Tufts College Methods of preparing substituted tetracyclines with transition metal-based chemistries
EA016099B1 (en) 1999-09-14 2012-02-28 Трастис Оф Тафтс Коллидж Substituted tetracycline compound (embodiments) and method of preparing thereof
CN1430600A (en) 2000-03-31 2003-07-16 塔夫茨大学信托人 7-and 9-carbamate, urea, thiourea, thiocarbamate and heteroaryl-amino substituted tetracycline compounds
JP2003533504A (en) * 2000-05-15 2003-11-11 パラテック ファーマシューティカルズ インコーポレイテッド 7-substituted fused ring tetracycline compound
BRPI0112269B8 (en) * 2000-07-07 2021-05-25 Paratek Pharm Innc 9-aminomethyl substituted minocycline compound, and pharmaceutical composition
US7094806B2 (en) 2000-07-07 2006-08-22 Trustees Of Tufts College 7, 8 and 9-substituted tetracycline compounds
EP1241160A1 (en) 2001-03-13 2002-09-18 Glaxo Group Limited Tetracycline derivatives and their use as antibiotic agents
EP2301914A1 (en) 2001-03-13 2011-03-30 Paratek Pharmaceuticals, Inc. 7,9-Substituted tetracycline compounds
US7553828B2 (en) 2001-03-13 2009-06-30 Paratek Pharmaceuticals, Inc. 9-aminomethyl substituted minocycline compounds
WO2002072506A2 (en) 2001-03-13 2002-09-19 Paratek Pharmaceuticals, Inc. 7-pyrollyl tetracycline compounds and methods of use thereof
WO2002085303A2 (en) * 2001-04-24 2002-10-31 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for the treatment of malaria
EP2332546A1 (en) 2001-07-13 2011-06-15 Paratek Pharmaceuticals, Inc. Tetracyclines for the treatment of stroke
WO2003055441A2 (en) 2001-08-02 2003-07-10 Paratek Pharmaceuticals, Inc. Medicaments
EP1474380A4 (en) 2002-01-08 2007-04-18 Paratek Pharm Innc 4-dedimethylamino tetracycline compounds
CN101307017A (en) * 2002-03-08 2008-11-19 帕拉特克药品公司 Amino-methyl substituted tetracycline compounds
AU2004259659B2 (en) 2003-07-09 2011-11-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
UA83266C2 (en) * 2003-12-08 2008-06-25 Уайет Oxazole derivatives of tetracyclines
JP5242161B2 (en) 2004-05-21 2013-07-24 プレジデント アンド フェローズ オブ ハーバード カレッジ Synthesis of tetracyclines and their analogs.
US7534766B2 (en) 2004-11-05 2009-05-19 Wyeth Glucuronide metabolites and epimers thereof of tigecycline
AR057649A1 (en) 2005-05-27 2007-12-12 Wyeth Corp SOLID CRYSTALINE TIGECICLINE FORMS AND METHODS TO PREPARE THE SAME
RU2008108215A (en) * 2005-08-31 2009-10-10 Вайет (Us) 9-AMINOCARBONYL SUBSTITUTED DERIVATIVES OF GLYCYCLICLINS
EP2026776A2 (en) 2006-05-15 2009-02-25 Paratek Pharmaceuticals, Inc. Methods of regulating expression of genes or of gene products using substituted tetracycline compounds
KR101178319B1 (en) 2007-11-29 2012-09-07 액테리온 파마슈티칼 리미티드 Phosphonic acid derivates and their use as p2y12 receptor antagonists
PT2271348T (en) 2008-03-28 2018-04-16 Paratek Pharm Innc FORMULATION OF ORAL TETRACYCIN COMPOUND TABLET
ITMI20080807A1 (en) 2008-05-05 2009-11-06 Antibioticos Spa PROCEDURE FOR THE PREPARATION OF TIGECYCLINE IN THE AMORPHOUS FORM
TW202332671A (en) 2008-05-19 2023-08-16 美商Ｐｒｔｋ Ｓｐｖ２公司 Tosylate salts and polymorphs of a tetracycline compound
HUE026562T2 (en) * 2008-08-08 2016-06-28 Tetraphase Pharmaceuticals Inc C7-fluoro substituted tetracycline compounds
US9073829B2 (en) 2009-04-30 2015-07-07 President And Fellows Of Harvard College Synthesis of tetracyclines and intermediates thereto
PL2427425T3 (en) 2009-05-08 2017-08-31 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
WO2011025982A2 (en) 2009-08-28 2011-03-03 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
KR101799304B1 (en) 2010-05-12 2017-11-20 렘펙스 파머수티클스 인코퍼레이티드 Tetracycline compositions
WO2013013504A1 (en) * 2011-07-26 2013-01-31 山东亨利医药科技有限责任公司 Tigecycline derivative
CA2883238C (en) 2012-08-31 2021-11-23 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
WO2015071299A2 (en) 2013-11-12 2015-05-21 Galenicum Health S.L. Stable pharmaceutical compositions
PH12019500822B1 (en) 2016-10-19 2024-02-21 Tetraphase Pharmaceuticals Inc Crystalline forms of eravacycline

Family Cites Families (2)

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Publication number Priority date Publication date Assignee Title
US3338963A (en) * 1960-10-28 1967-08-29 American Cyanamid Co Tetracycline compounds
US3579579A (en) * 1968-04-18 1971-05-18 American Cyanamid Co Substituted 7- and/or 9-amino-6-demethyl-6-deoxytetracyclines

Also Published As

Publication number Publication date
BR1100853A (en) 1999-12-07
AU654049B2 (en) 1994-10-20
CZ309397A3 (en) 1998-09-16
IL119590A (en) 1999-03-12
TW275616B (en) 1996-05-11
NL300244I2 (en) 2007-01-02
ZA927607B (en) 1993-04-13
FI114911B (en) 2005-01-31
DE69232302T2 (en) 2002-08-14
CZ284209B6 (en) 1998-09-16
DK0536515T3 (en) 2002-04-08
CA2079692A1 (en) 1993-04-05
MX9205532A (en) 1993-04-01
NZ244585A (en) 1995-07-26
NL300244I1 (en) 2007-01-02
IL103320A (en) 1998-12-06
PL173311B1 (en) 1998-02-27
ATE211128T1 (en) 2002-01-15
HU219973B (en) 2001-10-28
HU9203110D0 (en) 1992-12-28
SK298492A3 (en) 1995-03-08
HUT63145A (en) 1993-07-28
NO2006015I2 (en) 2011-03-14
CZ298492A3 (en) 1993-05-12
ES2168254T3 (en) 2002-06-16
NO2006015I1 (en) 2006-11-27
NO2017037I2 (en) 2017-08-01
CN1048240C (en) 2000-01-12
JPH05255219A (en) 1993-10-05
SK280837B6 (en) 2000-08-14
HK1011348A1 (en) 1999-07-09
CZ284159B6 (en) 1998-08-12
AU2618392A (en) 1993-04-08
CL2004001623A1 (en) 2005-06-03
LU91279I2 (en) 2006-12-11
NO301472B1 (en) 1997-11-03
EP0536515A1 (en) 1993-04-14
SK114999A3 (en) 2000-07-11
IL119590A0 (en) 1997-02-18
PL176333B1 (en) 1999-05-31
PL172282B1 (en) 1997-08-29
DE122006000058I1 (en) 2007-01-18
FI924454L (en) 1993-04-05
CN1072172A (en) 1993-05-19
KR100269072B1 (en) 2000-10-16
EP0536515B1 (en) 2001-12-19
DE69232302T4 (en) 2003-02-13
DE122006000058I2 (en) 2007-09-13
CA2079692C (en) 2004-06-08
NO923857L (en) 1993-04-05
IL103320A0 (en) 1993-03-15
HU211172A9 (en) 1995-11-28
PL175957B1 (en) 1999-03-31
SK284826B6 (en) 2005-12-01
NO923857D0 (en) 1992-10-02
DE69232302D1 (en) 2002-01-31
FI924454A0 (en) 1992-10-02
KR930007894A (en) 1993-05-20
SG52361A1 (en) 1998-09-28
JP3186863B2 (en) 2001-07-11
NO2017037I1 (en) 2017-08-01
PL296143A1 (en) 1993-05-31

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